Leishmanicidal, antifungal, and cytotoxic activity of triterpenoid glycosides isolated from the sea cucumber Neothyone gibbosa

Abstract

Neothyosides A - C, isolated from the body walls of the sea cucumber Neothyone gibbosa Deichmann, and a partially purified mixture of these saponins, were tested in vitro against promastigotes of two strains of Leishmania mexicana and a panel of several fungi using the broth microdilution technique. In addition, the cytotoxicity of these saponins was tested against Artemia salina. The IR, 1H and 13C NMR spectroscopic and FAB MS data of neothyoside C revealed that its structure was identical to that of pervicoside B, isolated from another sea cucumber species, Holothuria pervicax. Neothyoside C was the most active antiparasitic compound, inhibiting 100% of the promastigotes at 5 and 10 μg/mL of both L. mexicana strains. The mixture of saponins and pure neothyoside C showed the best activity against Aspergillus niger strains with MIC values between 15.6 μg/mL and 16.7 μg/mL for the mixture, and 4.65 μg/mL and 7.8 μg/mL for neothyoside C. Assays for cytotoxicity using Artemia salina showed that neothyosides A and C caused 50% brine-shrimp deaths at 130 and 63 μg/mL with this cytotoxicity 4 to 6 times greater than the concentration at which these compounds produce an antimicrobial effect. This is the first report describing the antileishmanial, antifungal, and cytotoxic activity of N. gibbosa saponins.